HIV-1 inhibitor-25

HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS[1].

Signaling Pathways >> Anti-infection >> HIV

Research Areas >> Infection

HIV (IIIB):13.6 nM (EC50)

HIV-1 (L100I):1.2458 ± 0 μM (EC50)

HIV-1 (K103N):0.4383 ± 0 μM (EC50)

HIV-1 (Y181C):0.5075 ± 0 μM (EC50)

HIV-1 (Y188L):5.8136 ± 2 μM (EC50)

HIV-1 (E138K):0.1961 ± 0 μM (EC50)

HIV-1 (F227L+V106A):3.0683 ± 0 μM (EC50)

[1]. Chen X, et al. Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. Eur J Med Chem. 2020;202:112549.